BRPI0411868B8 - derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase - Google Patents

derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase

Info

Publication number
BRPI0411868B8
BRPI0411868B8 BRPI0411868A BRPI0411868A BRPI0411868B8 BR PI0411868 B8 BRPI0411868 B8 BR PI0411868B8 BR PI0411868 A BRPI0411868 A BR PI0411868A BR PI0411868 A BRPI0411868 A BR PI0411868A BR PI0411868 B8 BRPI0411868 B8 BR PI0411868B8
Authority
BR
Brazil
Prior art keywords
pyrrole
pyrazole derivatives
kinase inhibitors
derivatives active
active
Prior art date
Application number
BRPI0411868A
Other languages
English (en)
Inventor
Forte Barbara
Fancelli Daniele
Moll Jurgen
Varasi Mario
Vianello Paola
Original Assignee
Nerviano Medical Science S R L
Pfizer Italia Srl
Pharmacia Italia Spa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Nerviano Medical Science S R L, Pfizer Italia Srl, Pharmacia Italia Spa filed Critical Nerviano Medical Science S R L
Publication of BRPI0411868A publication Critical patent/BRPI0411868A/pt
Publication of BRPI0411868B1 publication Critical patent/BRPI0411868B1/pt
Publication of BRPI0411868B8 publication Critical patent/BRPI0411868B8/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Abstract

"derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase. a presente invenção refere-se a derivados de pirrol[3,4-c]pirazol de fórmula i e seus sais farmaceuticamente aceitáveis, como definido no relatório descritivo, processo para sua preparação e composições farmacêuticas compreendendo-os; os compostos da invenção podem ser úteis em terapia no tratamento de doenças associadas com uma atividade de proteína cinase desregulada, como câncer.
BRPI0411868A 2003-07-09 2004-07-08 derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase BRPI0411868B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48581403P 2003-07-09 2003-07-09
PCT/EP2004/007515 WO2005005427A1 (en) 2003-07-09 2004-07-08 PYRROLO[3,4-c]PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS

Publications (3)

Publication Number Publication Date
BRPI0411868A BRPI0411868A (pt) 2006-08-08
BRPI0411868B1 BRPI0411868B1 (pt) 2019-11-12
BRPI0411868B8 true BRPI0411868B8 (pt) 2021-05-25

Family

ID=34062099

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0411868A BRPI0411868B8 (pt) 2003-07-09 2004-07-08 derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase

Country Status (42)

Country Link
US (2) US7141568B2 (pt)
EP (1) EP1644376B1 (pt)
JP (1) JP4728232B2 (pt)
KR (1) KR101075711B1 (pt)
CN (1) CN100564380C (pt)
AP (1) AP2214A (pt)
AR (1) AR050045A1 (pt)
AT (1) ATE480540T1 (pt)
AU (1) AU2004255347B2 (pt)
BR (1) BRPI0411868B8 (pt)
CA (1) CA2531759C (pt)
CR (1) CR8171A (pt)
CY (1) CY1110832T1 (pt)
DE (1) DE602004029045D1 (pt)
DK (1) DK1644376T3 (pt)
DO (1) DOP2004000949A (pt)
EA (1) EA009462B1 (pt)
EC (1) ECSP056246A (pt)
ES (1) ES2349780T3 (pt)
GE (1) GEP20084395B (pt)
GT (2) GT200400133AA (pt)
HK (1) HK1089769A1 (pt)
HN (1) HN2004000232A (pt)
IL (1) IL172923A (pt)
IS (1) IS2843B (pt)
MA (1) MA28064A1 (pt)
ME (1) MEP51908A (pt)
MX (1) MXPA06000362A (pt)
MY (1) MY139072A (pt)
NO (1) NO332361B1 (pt)
NZ (1) NZ544514A (pt)
PA (1) PA8606201A1 (pt)
PE (1) PE20050325A1 (pt)
PL (1) PL1644376T3 (pt)
PT (1) PT1644376E (pt)
RS (2) RS52155B (pt)
SI (1) SI1644376T1 (pt)
TN (1) TNSN06009A1 (pt)
TW (1) TWI343382B (pt)
UA (1) UA81682C2 (pt)
WO (1) WO2005005427A1 (pt)
ZA (1) ZA200600095B (pt)

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WO2006023931A2 (en) * 2004-08-18 2006-03-02 Takeda San Diego, Inc. Kinase inhibitors
US7713973B2 (en) * 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
BRPI0518509A2 (pt) * 2005-01-10 2008-11-25 Pfizer pirrolopirazàis, inibidores de cinase potentes
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
TW200808311A (en) 2006-03-30 2008-02-16 Nerviano Medical Sciences Srl Use of a kinase inhibitor for the treatment of particular resistant tumors
WO2008017465A1 (en) * 2006-08-10 2008-02-14 F. Hoffmann-La Roche Ag Bicyclic lactam derivatives, their manufacture and use as pharmaceutical agents
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
WO2008052931A1 (en) * 2006-11-03 2008-05-08 Nerviano Medical Sciences S.R.L. A method of administering an antitumor compound
AR071780A1 (es) * 2008-05-15 2010-07-14 Nerviano Medical Sciences Srl Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos
US20110129467A1 (en) * 2008-07-24 2011-06-02 Nerviano Medical Sciences S.R.L. Therapeutic combination comprising an aurora kinase inhibitor and antiproliferative agents
JP5518062B2 (ja) * 2008-07-24 2014-06-11 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ オーロラキナーゼ阻害剤および抗悪性腫瘍剤を含む治療用組み合わせ
US20100022553A1 (en) * 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib
US20100183601A1 (en) 2008-12-22 2010-07-22 Millennium Pharmaceuticals, Inc. Combination of Aurora Kinase Inhibitors and Anti-CD20 Antibodies
EA025352B1 (ru) 2011-12-12 2016-12-30 Др. Редди'С Лабораториз Лтд. ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ТРОПОМИОЗИН-РЕЦЕПТОРНОЙ КИНАЗЫ (Trk)
CN104072498B (zh) * 2013-03-26 2016-12-28 沈阳药科大学 (R)‑N‑[5‑(2‑甲氧基‑2‑苯基乙酰基)‑1,4,5,6‑四氢吡咯并[3,4‑c]吡唑‑3‑基]‑4‑(4‑甲基哌嗪‑1‑基)苯甲酰胺的合成方法
JP6525474B2 (ja) 2013-12-06 2019-06-05 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. オーロラキナーゼ阻害剤と抗cd30抗体の併用
US9394305B2 (en) 2014-06-23 2016-07-19 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds as tropomyosin receptor kinase a (TrkA) inhibitors
CN107735401B (zh) 2015-06-15 2021-08-31 宇部兴产株式会社 取代二氢吡咯并吡唑衍生物
CN107337674B (zh) * 2016-04-29 2019-09-20 江苏吉贝尔药业股份有限公司 用于dpp-iv抑制剂的四氢吡喃胺衍生物、其药物组合物和制剂以及用途
US11874276B2 (en) 2018-04-05 2024-01-16 Dana-Farber Cancer Institute, Inc. STING levels as a biomarker for cancer immunotherapy
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
CN113563346A (zh) * 2021-08-19 2021-10-29 守恒(厦门)医疗科技有限公司 吡咯[3,4-c]并吡唑二酰胺类衍生物及其在抗肿瘤药物中的应用
WO2023196959A1 (en) 2022-04-07 2023-10-12 Eli Lilly And Company Process for making a kras g12c inhibitor
WO2023196887A1 (en) 2022-04-08 2023-10-12 Eli Lilly And Company Method of treatment including kras g12c inhibitors and aurora a inhibitors
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Also Published As

Publication number Publication date
CA2531759C (en) 2013-04-02
EA009462B1 (ru) 2007-12-28
US7141568B2 (en) 2006-11-28
DK1644376T3 (da) 2011-01-03
RS52155B (en) 2012-08-31
MXPA06000362A (es) 2006-03-28
ZA200600095B (en) 2007-01-31
NO332361B1 (no) 2012-09-03
JP4728232B2 (ja) 2011-07-20
BRPI0411868B1 (pt) 2019-11-12
IL172923A0 (en) 2006-06-11
AU2004255347B2 (en) 2010-04-08
MY139072A (en) 2009-08-28
GT200400133A (es) 2005-04-18
ATE480540T1 (de) 2010-09-15
GT200400133AA (es) 2007-07-10
UA81682C2 (en) 2008-01-25
IL172923A (en) 2011-09-27
PL1644376T3 (pl) 2011-03-31
US20060276471A1 (en) 2006-12-07
TWI343382B (en) 2011-06-11
SI1644376T1 (sl) 2010-11-30
PT1644376E (pt) 2010-09-24
PA8606201A1 (es) 2005-08-04
CN100564380C (zh) 2009-12-02
EA200600209A1 (ru) 2006-06-30
EP1644376B1 (en) 2010-09-08
NZ544514A (en) 2009-07-31
HN2004000232A (es) 2011-01-17
CA2531759A1 (en) 2005-01-20
GEP20084395B (en) 2008-06-10
NO20060113L (no) 2006-04-05
RS20060004A (en) 2008-06-05
ES2349780T3 (es) 2011-01-11
AR050045A1 (es) 2006-09-27
US20050032839A1 (en) 2005-02-10
EP1644376A1 (en) 2006-04-12
DE602004029045D1 (de) 2010-10-21
HK1089769A1 (en) 2006-12-08
IS2843B (is) 2013-08-15
AP2214A (en) 2011-03-04
JP2009513525A (ja) 2009-04-02
CY1110832T1 (el) 2015-06-10
ECSP056246A (es) 2006-04-19
AP2006003480A0 (en) 2006-02-28
KR101075711B1 (ko) 2011-10-21
CN1820009A (zh) 2006-08-16
DOP2004000949A (es) 2005-01-15
IS8192A (is) 2005-12-22
KR20060033001A (ko) 2006-04-18
MA28064A1 (fr) 2006-08-01
BRPI0411868A (pt) 2006-08-08
TNSN06009A1 (fr) 2007-10-03
TW200510385A (en) 2005-03-16
US7582628B2 (en) 2009-09-01
WO2005005427A1 (en) 2005-01-20
CR8171A (es) 2006-08-09
PE20050325A1 (es) 2005-05-17
AU2004255347A1 (en) 2005-01-20
MEP51908A (en) 2011-05-10

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